Janssen Pharmaceutica Nv

Janssen Pharmaceutica

Jan Vandenberk

Ludo E Kennis

Marcel J Van Der Aa

Albert H Van Heertum

Josephus Carolus Mertens

Jozef M Boey

Alfonsus G Knaeps

Albertus H Van Heertum

Ludo Edmond Josephine Kennis

Cornelus G Janssen

Paul A Janssen

Jozef F Hens

Cornelus Gerardus Maria Janssen

Ineke Van Wijngaarden

Albertus Henricus Maria Theresia Van Heertum

Willem Soudijn

4-&lsqb;3-benzofuranyl&rsqb;piperidinyl and 4-&lsqb;3-benzothienyl&rsqb;piperidinyl derivatives

There is disclosed a process for preparing an enantiomeric form of the compound having the formula:

3-piperidinyl-1,2-benzisoxazoles

4-(1H-indol-1-yl)-1-piperidinyl derivatives

9-Hydroxy-pyrido�1,2-a!pyrimidin-4-one ether derivatives

Novel 2,9-disubstituted-4H-pyrido[1,2-a]pyrimidin-4-ones having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein Alk represents C.sub.1-4 alkanediyl, D is a bicyclic heterocycle of formula ##STR2## wherein R.sup.1 represents C.sub.1-4 alkyl, hydroxyC.sub.1-4 alkyl, carboxaldehyde, carboxyl, C.sub.1-10 alkylcarbonyloxyC.sub.1-4 alkyl; each R.sup.2 represents hydrogen or C.sub.1-4 alkyl; R.sup.3 represents C.sub.1-4 alkyl, hydroxyC.sub.1-4 alkyl or methyl substituted with phenyl, 5-methyl-2-furanyl or 3-pyridinyl; and R.sup.4 represents C.sub.1-3 alkyl, phenyl, 5-methyl-2-furanyl or 3-pyridinyl.

(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl-alkyl-(2,

3-Piperidinyl-indazole derivatives and their pharmaceutically acceptable acid addition salts being useful antagonists of neurotransmitters; pharmaceutical compositions containing the same and a method of treating warm-blooded animals suffering from diseases associated with the release of said neutrotransmitters.

Antihypertensive 3-piperidinyl-indazole derivatives

2-Amino-pyrimidininone derivatives possessing serotonin-antagonistic and anti-histaminic properties. Compositions containing these compounds as the active ingredient. Method of treating subjects suffering from diseases and/or disorders associated with the release of neurotransmitters, in particular, a method of treating subjects suffering form sleep disorders with 2-aminopyrimidinone derivatives substituted with a 4-bis(aryl)methylene-1-piperidinyl group; and a method of treating subjects suffering from psychotic diseases and/or disorders with 2-aminopyrimidinone derivatives substituted with a 4-arylcarbonyl-1-piperidinyl, 4-benzazolyl-1-piperidinyl, 4-benzazolyl-1-piperazinyl or 4-indolyl-1-piperidinyl, 4-benzo[b]furanyl-1-piperidinyl or 4-benzo[b]thienyl-1-piperidinyl group.

2-aminopyrimidinone derivatives

2-Amino-pyrimidininone derivatives possessing serotonin-antagonistic and antihistaminic properties. Compositions containing these compounds as the active ingredient. Method of treating subjects suffering from diseases and/or disorders associated with the release of neurotransmitters, in particular, a method of treating subjects suffering from sleep disorders with 2-aminopyrimidinone derivatives substituted with a 4-bis(aryl)methylene-1-piperidinyl group; and a method of treating subjects suffering from psychotic diseases and/or disorders with 2-aminopyrimidinone derivatives substituted with a 4-arylcarbonyl-1-piperidinyl, 4-benzazolyl-1-piperidinyl, 4-benzazolyl-1-piperazinyl or 4-indolyl-1-piperidinyl, 4-benzo[b]furanyl-1-piperidinyl or 4-benzo[b]thienyl-1-piperidinyl group.

The invention relates to C.sub.2-20 alkanoic acid esters of 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6, 7,8,9-tetrahydro-9-hydroxy-2 -methyl-4H-pyrido[1,2-a]pyrimidin-4-one, pharmaceutically acceptable acid addition salts thereof, and enantiomeric forms thereof, which are useful in the treatment of warm-blooded animals suffering from psychotic diseases.

The present invention relates to novel 3-piperidinyl-1,2-benzisoxazoles having long-acting antipsychotic properties and which are useful in the treatment of warm-blooded animals suffering from psychotic diseases. Methods of preparing said compounds and compositions containing the same.

3-[2-[4-(6-fluoro-1,2-benzisoxozol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9

2-Amino-pyrimidininone derivatives possessing serotonin-antagonistic and antihistaminic properties. Compositions containing these compounds as the active ingredient. Method of treating subjects suffering from diseases and/or disorders associated with the release of neurotransmitters, in particular, a method of treating subjects suffering from sleep disorders with 2-aminopyrimidinone derivatives substituted with a 4-bis(aryl)methylene-1-piperidinyl group; and a method of treating subjects suffering from psychotic diseases and/or disorders with 2-aminopyrimidinone derivatives substituted with a 4-arylcarbonyl-1-piperidinyl, 4-benzazoyl-1-piperidinyl, 4-benzazolyl-1-piperazinyl or 4-indolyl-1-piperidinyl, 4-benzo[b]furanyl-1-piperidinyl or 4-benzo[b]thienyl-1-piperidinyl group.

3-Piperazinyl-1,2-benzazoles and their pharmaceutically acceptable acid addition salts having useful antipsychotic properties and being useful in the treatment of a variety of disorders in which serotonin and/or dopamine release is of predominant importance.

Antipsychotic 3-piperazinylbenzazole derivatives

3-Piperdinyl-1,2-benzisothiazoles and 3-piperidinyl-1,2-benzisoxazoles and their pharmaceutically acceptable acid addition salts having useful antipsychotic properties and being useful in the treatment of a variety of complaints in which serotonin release is of predominant importance.

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Beerse, Belgium

Jan Vandenberk